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    Chemistry

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    Also known as: 916072-89-4, S-297995, 03ksi6wlxh, S 297995, S-297,995, (4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-n-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide
    Molecular Formula
    C32H34N4O6
    Molecular Weight
    570.6  g/mol
    InChI Key
    AXQACEQYCPKDMV-RZAWKFBISA-N
    FDA UNII
    03KSI6WLXH
    Naldemedine
    Naldemedine is an opioid receptor antagonist. It is a modified form of [DB00704] to which a side chain has been added to increase molecular weight and polar surface area resulting in restricted transport across the blood brain barrier. Naldemedine was approved in 2017 in both the US and Japan for the treatment of Opioid-induced Constipation.
    Naldemedine is an Opioid Antagonist. The mechanism of action of naldemedine is as an Opioid Antagonist.
    1 2D Structure

    Naldemedine

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    (4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-N-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide
    2.1.2 InChI
    InChI=1S/C32H34N4O6/c1-30(2,29-33-27(35-42-29)18-6-4-3-5-7-18)34-28(39)20-15-32(40)22-14-19-10-11-21(37)25-23(19)31(32,26(41-25)24(20)38)12-13-36(22)16-17-8-9-17/h3-7,10-11,17,22,26,37-38,40H,8-9,12-16H2,1-2H3,(H,34,39)/t22-,26+,31+,32-/m1/s1
    2.1.3 InChI Key
    AXQACEQYCPKDMV-RZAWKFBISA-N
    2.1.4 Canonical SMILES
    CC(C)(C1=NC(=NO1)C2=CC=CC=C2)NC(=O)C3=C(C4C56CCN(C(C5(C3)O)CC7=C6C(=C(C=C7)O)O4)CC8CC8)O
    2.1.5 Isomeric SMILES
    CC(C)(C1=NC(=NO1)C2=CC=CC=C2)NC(=O)C3=C([C@H]4[C@@]56CCN([C@@H]([C@@]5(C3)O)CC7=C6C(=C(C=C7)O)O4)CC8CC8)O
    2.2 Other Identifiers
    2.2.1 UNII
    03KSI6WLXH
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl- 1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide

    2. S-297995

    3. Symproic

    2.3.2 Depositor-Supplied Synonyms

    1. 916072-89-4

    2. S-297995

    3. 03ksi6wlxh

    4. S 297995

    5. S-297,995

    6. (4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,7,9-trihydroxy-n-[2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl]-1,2,4,5,7a,13-hexahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamide

    7. Naldemedine [usan]

    8. Unii-03ksi6wlxh

    9. Naldemedine [usan:inn]

    10. Naldemedine [mi]

    11. Naldemedine [inn]

    12. Naldemedine (usan/inn)

    13. Naldemedine [who-dd]

    14. Gtpl9150

    15. Schembl9880572

    16. Chembl2105755

    17. Dtxsid501030350

    18. Bdbm50503604

    19. Db11691

    20. Compound 9k [pmid: 30446313]

    21. Hy-19627

    22. Morphinan-7-carboxamide, 17-(cyclopropylmethyl)-6,7-didehydro-4,5-epoxy-3,6,14- Trihydroxy-n-(1-methyl-1-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl)-,(5alpha)-

    23. Cs-0016072

    24. J3.573.009e

    25. D10188

    26. Q6960846

    27. 17-(cyclopropylmethyl)-6,7-didehydro-4,5a-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide

    28. 17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,6,14-trihydroxy-n-(2-(3-phenyl- 1,2,4-oxadiazol-5-yl)propan-2-yl)morphinan-7-carboxamide

    2.4 Create Date
    2011-12-27
    3 Chemical and Physical Properties
    Molecular Weight 570.6 g/mol
    Molecular Formula C32H34N4O6
    XLogP33.2
    Hydrogen Bond Donor Count4
    Hydrogen Bond Acceptor Count9
    Rotatable Bond Count6
    Exact Mass570.24783482 g/mol
    Monoisotopic Mass570.24783482 g/mol
    Topological Polar Surface Area141 Ų
    Heavy Atom Count42
    Formal Charge0
    Complexity1140
    Isotope Atom Count0
    Defined Atom Stereocenter Count4
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 1  
    Drug NameSYMPROIC
    Active IngredientNALDEMEDINE TOSYLATE
    CompanySHIONOGI INC (Application Number: N208854. Patents: 9108975, RE46365, RE46375)

    4.2 Drug Indication

    For the treatment of opioid-induced constipation.

    FDA Label

    Rizmoic is indicated for the treatment of opioid-induced constipation (OIC) in adult patients who have previously been treated with a laxative.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Naldemedine is an opioid receptor antagonist with restricted movement across the blood brain barrier. This allows it to antagonize the periperal effects of opioid drugs such as constipation without interfering with the effects on the central nervous system.

    5.2 FDA Pharmacological Classification
    5.2.1 Active Moiety
    NALDEMEDINE
    5.2.2 FDA UNII
    03KSI6WLXH
    5.2.3 Pharmacological Classes
    Opioid Antagonists [MoA]; Opioid Antagonist [EPC]
    5.3 ATC Code

    A06AH05

    A - Alimentary tract and metabolism

    A06 - Drugs for constipation

    A06A - Drugs for constipation

    A06AH - Peripheral opioid receptor antagonists

    A06AH05 - Naldemedine

    5.4 Absorption, Distribution and Excretion

    Absorption

    Tmax is 0.75 h. Administration with a high-fat meal reduces Cmax by 35% and increases Tmax to 2.5 h.

    Route of Elimination

    57% of naldemedine is excreted in the urine with 16-18% as the parent compound and 35% is excreted in the feces.

    Volume of Distribution

    The apparent volume of disribution during the terminal phase is 155 L

    5.5 Metabolism/Metabolites

    Naldemedine is mainly metabolized to nor-naldemedine by CYP3A. Some metabolism to naldemedine-3-glucuronide occurs via UGT1A3. Both metabolites are acitive but less potent than naldemedine. The relative exposures of these metabolites are 9-13% and <3% for nor-naldemedine and naldemedine-3-glucuronide respectively. Naldemedine is also cleaved in the intestine to form benzamidine and naldemedine carboxylic acid.

    5.6 Biological Half-Life

    The terminal elimination half life is 11 h.

    5.7 Mechanism of Action

    Naldemedine binds to and antagonizes mu-, delta-, and kappa-opioid receptors. The binding of opioid agonists to peripheral mu-opioid receptors slows the transit of feces through the intestine resulting in constipation. By antagonizing mu-opioid receptors, naldemedine inhibits this effect.

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